Target intelligence / Profile preview

Type 3 Cyclic Nucleotide Phosphodiesterase (PDE3)

Target
PDE3
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

Type 3 cyclic nucleotide phosphodiesterases (PDE3) are a family of enzymes that hydrolyze the second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), thereby regulating their intracellular concentrations and modulating various physiological processes. PDE3 is also known as cGMP-inhibited phosphodiesterase due to its unique regulatory mechanism. Acute use of selective PDE3 inhibitors increases cardiac output via positive inotropic effects. However long-term use raises mortality risk due to arrhythmias/sudden death. Downregulation or dysfunction may contribute to progression of heart failure.

Other names
cGMP-inhibited phosphodiesterase
02

Mechanism of action

Selective PDE3 inhibitors increase cardiac output via positive inotropic effects and modulate vasodilation through effects on cAMP/cGMP signaling.

03

Biological functions

Hydrolysis of cAMPHydrolysis of cGMPRegulation of cAMP levelsRegulation of cGMP levelsRegulation of contractilityModulation of vasodilationSignal transduction
04

Disease associations

Heart FailureCardiovascular disease
05

Safety considerations

Increased risk of arrhythmias or sudden death with chronic inhibition
06

Interacting drugs

Milrinone

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